| Bioactivity | PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC50 of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells[1]. |
| Invitro | PLK1-IN-6 (compound 21 g) 对四种肿瘤来源的细胞系显示出显着的抗增殖活性 (MCF-7 IC50=8.64 nM, HCT-116 IC50=26.0 nM, MDA-MB-231 IC50=14.8 nM and MV4-11 IC50=47.4 nM)[1] .PLK1-IN-6 代谢适中，在人肝微粒体中的半衰期为 25.7 min[1]。 |
| In Vivo | PLK1-IN-6 (compound 21 g) (1 mg/kg; i.v.) 在 Sprague Dawley 大鼠中表现出良好的半衰期 (10.1 h) 和血浆浓度曲线下面积[1]。PLK1-IN-6 (10 mg/kg; i.g.) 在 Sprague Dawley 大鼠中表现出低清除率值和高血浆暴露量 (26800 ng•h/mL)，具有良好的生物利用度 (11.4%)[1]。PLK1-IN-6 (10 mg/kg; i.g.) 在 Balb/c 小鼠中表现出长半衰期 (2.73 h)，高血浆暴露 (11227 ng•h/mL) 和出色的生物利用度 (77.4%)[ 1]。PLK1-IN-6 (20 mg/kg; i.g.) 对小鼠没有明显的毒性[1]。 |
| Name | PLK1-IN-6 |
| Formula | C28H37N9O3 |
| Molar Mass | 547.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Li Z, et, al. Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1. Eur J Med Chem. 2023 May 5;251:115242. |